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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
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The Synthesis and Transfection Activity of Disulfide Polycationic Amphiphiles
I A Petukhov1, P A Puchkov1, N G Morozova1
1Lomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119571 Moscow, Russia.
Russian Journal of Bioorganic Chemistry
|May 16, 2023
Summary
New polycationic amphiphiles form non-toxic liposomes for efficient gene delivery. These novel cationic liposomes show promise for both in vitro transfection and in vivo studies.
Area of Science:
- Biochemistry
- Materials Science
- Molecular Biology
Background:
- Developing safe and effective non-viral gene delivery vectors is crucial for gene therapy.
- Polycationic amphiphiles offer potential for forming liposomal carriers.
- Disulfide bonds can be incorporated to enable payload release.
Purpose of the Study:
- To synthesize novel polycationic amphiphiles with disulfide groups.
- To evaluate the efficacy and toxicity of liposomes formed from these amphiphiles for nucleic acid delivery.
- To investigate the influence of amphiphile structure on transfection efficiency.
Main Methods:
- Synthesis of novel polycationic amphiphiles containing disulfide bonds.
- Formation of cationic liposomes using synthesized amphiphiles and helper lipids (e.g., DOPE).
- In vitro transfection assays using fluorescently labeled oligodeoxyribonucleotides and plasmid DNA in HEK293 and HeLa cells.
- Cell viability assays to assess liposome toxicity.
Main Results:
- Synthesized polycationic amphiphiles successfully formed cationic liposomes.
- Liposomes exhibited no toxicity towards HEK293 and HeLa cells.
- High efficiency was observed for delivering oligodeoxyribonucleotides.
- Plasmid DNA delivery efficiency varied with cell line and amphiphile structure, with tetracationic amphiphiles being most effective.
Conclusions:
- Novel polycationic amphiphiles can form safe and effective liposomal gene delivery systems.
- These liposomes demonstrate potential for in vitro transfection of eukaryotic cells.
- The developed liposomes warrant further investigation for in vivo applications.

